Lecithin microemulsions for the topical administration of ketoprofen: percutaneous adsorption through human skin and in vivo human skin tolerability

Paolino, Donatella; Ventura, Cinzia Anna; Nisticò, Steven Paul; Puglisi, Giovanni; Fresta, Massimo

doi:10.1016/s0378-5173(02)00295-8

Cited by 174 publications

(99 citation statements)

References 25 publications

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“…In the last decade, studies suggested that phospholipid microemulsions produce enhanced transdermal flux for oilsoluble drugs (Dreher et al, 1997;Paolino et al, 2002;Peltola et al, 2003). However, the potential of phospholipidbased microemulsion have never been explored in cutaneous delivery of local anesthetics.…”

Section: Introductionmentioning

confidence: 99%

Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

et al. 2014

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Topical delivery of local anesthetics has been an area of interest for researchers considering the barrier properties of skin and unfavorable physicochemical properties of drugs. In the present study, efforts have been made to modify the in vivo efficacy of eutectic mixture of lidocaine and prilocaine by exploiting the phospholipid modified microemulsion based delivery systems. The strategic QbD (D-optimal mixture design) enabled systematic optimization approach, after having obtained the isotropic area of interest by ternary phase diagram, has resulted into the system with most desirable attributes. Latter include nano-scale, globular structures with an average size of 40.6 nm, as characterized by TEM and DLS. The optimized microemulsion systems in gel dosage forms revealed the better permeability over commercial cream (CC) through abdominal rat skin. Enhancement in the flux from M OPT-NMP gel was 3.22-folds for prilocaine and 4.94-folds for lidocaine, in comparison to that of CC. This enhanced skin permeability is very well reflected in the in vivo studies, wherein intensity and duration of action was augmented significantly. The skin compliance of the optimized formulation was revealed in histopathological studies. The overall benefit relating to efficacy and safety-compliance could be correlated to the uniqueness of the carriers, composed of phospholipids and other components. Hence, the developed phospholipid-microemulsion based gel formulation has been proposed as more useful alternative for the topical delivery of lidocaine and prilocaine.

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Section: Introductionmentioning

confidence: 99%

Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

et al. 2014

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“…Different Smix ratios 1:1, 1:2, 1:3, 2:1, 3:1, and 4:1. The ratio [9][10][11] was selected in different concentration. Firstly concentration of surfactant was increased as compared to Co-surfactant and in second condition concentration of Co-surfactant was increased as compared to surfactant, different ratio of oil and Smix were varied as 9.5:0.5, 9:1, 8.5:1.5, 8:2, 7.5:2.5, 7:3, 6.5:3.5, 6:4, 5.5:4.5, 5:5, 4.5:5.5, 4:6, 3.5:6.5, 3:7, 2.5:7.5, 2:8, 1.5:8.5, 1:9, 0.5:9.5 Were chosen so as to cover maximum ratio which will be important to define the ternary diagram.…”

Section: Construction Of Pseudo -Ternary Phase Diagrammentioning

confidence: 99%

Design Development and Evaluation of Topical Microemulsion

Muzaffar¹,

Singh²

2017

Int. Res. J. Pharm.

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A microemulsion based gel was designed for the topical and targeted delivery of sertaconazole nitrate for the treatment of su perficial fungal infection. The microemulsion region was obtained using a ternary diagram, different ratio of oil and Smix were used. The microemulsion of sertaconazole containing 2% (w/w) of sertaconazole, 6.67% (w/w) of oil phase (Eugenol+Oleic acid 1:1), 60.18% (w/w) of surfactant mixture 2:1 ratio (Tween-80 and Transcutol-P) and 33.15% (w/w) with distilled water. The prepared microemulsion gel and commercial cream of sertaconazole were evaluated for in-vitro and ex-vivo studies. The highest drug retention was achieved with Tween 80 and Transcutol P (T80TC45) when the optimized formulation was converted to a gel. The designed formulation MG2 was safe to be used over the skin as the PDI=0 when compared with commercial cream and MG1. The optimized formulation also posse's anti-inflammatory activity. The average zone of inhibition of MG2 was (23.19 ± 0.478) which was more than the commercial cream (15.34 ± 0.382) or MG1 (17.78 ± 0.715). Candida albicans which may be due to better permeation and retention effect of microemulsion gel 2. The MG2 was found to be stable after six month. The results obtained in this research from in vitro and in vivo data it can be concluded that the developed microemulsions have great potential for topical drug delivery in the treatment of inflammation and fungal infection.

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“…The irritant effect of formulations was investigated on healthy volunteers, and their safety was demonstrated. In another study, lecithin microemulsions of ketoprofen were developed (Paolino et al, 2002). Permeation of drug from microemulsion formulation was compared to the conventional dermal ketoprofen formulation.…”

Section: Novel Formulation Approaches For Improving Skin Delivery Of mentioning

confidence: 99%

Novel Formulation Approaches for Dermal and Transdermal Delivery of Non-Steroidal Anti-Inflammatory Drugs

Okyar¹,

Özsoy²,

Güngör³

2012

Rheumatoid Arthritis - Treatment

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Lecithin microemulsions for the topical administration of ketoprofen: percutaneous adsorption through human skin and in vivo human skin tolerability

Cited by 174 publications

References 25 publications

Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

Design Development and Evaluation of Topical Microemulsion

Novel Formulation Approaches for Dermal and Transdermal Delivery of Non-Steroidal Anti-Inflammatory Drugs

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